XL413 (hydrochloride)
- Product Name
- XL413 (hydrochloride)
- CAS No.
- 2062200-97-7
- Chemical Name
- XL413 (hydrochloride)
- Synonyms
- XL413 xhydrochloride;XL413 hydrochloride, 10 mM in DMSO;XL-413 hydrochloride,XL413 hydrochloride
- CBNumber
- CB14666854
- Molecular Formula
- C14H13Cl2N3O2
- Formula Weight
- 326.18
- MOL File
- 2062200-97-7.mol
XL413 (hydrochloride) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:0.2(Max Conc. mg/mL);0.613(Max Conc. mM)
PBS (pH:7.2):10.0(Max Conc. mg/mL);30.66(Max Conc. mM) - form
- A crystalline solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 24906
- Product name
- XL413 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $119
- Updated
- 2024/03/01
- Product number
- 24906
- Product name
- XL413 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $223
- Updated
- 2024/03/01
- Product number
- 24906
- Product name
- XL413 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $444
- Updated
- 2024/03/01
- Product number
- 24906
- Product name
- XL413 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $748
- Updated
- 2023/06/20
- Product number
- CS-1957
- Product name
- XL413 hydrochloride
- Purity
- 99.72%
- Packaging
- 5mg
- Price
- $144
- Updated
- 2021/12/16
XL413 (hydrochloride) Chemical Properties,Usage,Production
Description
XL413 is a potent inhibitor of Cdc7 (IC50 = 3.4 nM). It is >60, >10, and >300-fold selective for Cdc7 over CK2, PIM1, and a panel of over 100 protein kinases, respectively. XL413 inhibits the growth of MDA-MB-231T and COLO 205 cells (IC50s = 118 and 140 nM, respectively). It inhibits Cdc7-specific phosphorylation of mini-chromosome maintenance protein (MCM2) and induces cell cycle accumulation in the S and G2 phases in MDA-MB-231T and COLO 205 cells that overexpress Cdc7. In vivo, XL413 inhibits MCM2 phosphorylation (ED50 = <3 mg/kg) and reduces tumor growth in a COLO 205 mouse xenograft model when administered orally at doses of 10, 30, and 100 mg/kg.
Uses
XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
in vivo
XL413 (BMS-863233; 100 mg/kg, p.o.) hydrochloride shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) hydrochloride is well tolerated at all the doses, with no significant body weight loss[1].
IC 50
Cdc7: 3.4 nM (IC50); PIM1: 42 nM (IC50); CK2: 215 nM (IC50)
References
[1] Koltun ES, et al. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. DOI:10.1016/j.bmcl.2012.04.024
[2] Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300. DOI:10.1371/journal.pone.0113300
XL413 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
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